Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEAcrizanibCat.No.:HY-109020CASNo.:1229453-99-9Synonyms:LHA510分?式:C??H??F?N?O?分?量:445.4作?靶點:VEGFR作?通路:ProteinTyrosineKinase/RTK儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:41.67mg/mL(93.56mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.2452mL11.2259mL22.4517mL5mM0.4490mL2.2452mL4.4903mL10mM0.2245mL1.1226mL2.2452mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.08mg/mL(4.67mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(4.67mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.67mM);ClearsolutionBIOLOGICALACTIVITY?物活性Acrizanib(LHA510)?種VEGFR-2的抑制劑，其對BaF3-VEGFR-2的IC50值為17.4nM。IC50&TargetVEGFR-217.4nM(IC50)體外研究AcrizanibisaVEGFR-2inhibitor,withanIC50of17.4nMforBaF3-KDR.Acrizanib(compound35)exhibits≤10%remainingkinaseactivityagainstonly13wildtypekinases:CSF1R,Kit,PDGFRα,PDGFRβ,VEGFR1,VEGFR2,VEGFR3,Fms(solubleVEGFR1),DDR1,DDR2,TIE1,andABL1(nonphosphorylated)[1].體內(nèi)研究RatocularPKstudieswithAcrizanibshowsadistinctlydifferentprofilefromthatobservedwithcompound25.WhileprolongedexposureisonceagainevidentinthePEC,theAUCratiotothelevelofAcrizanibinplasmaismarkedlyincreased(>21000-foldhigherexposureinthePECthanplasmaonday11).Furthermore,unlike25,AcrizanibalsoaffordmuchimprovedretinatoplasmaAUCexposureratioafter10daysofdosing(598×forAcrizanibvs0.8×for25)[1].REFERENCES[1].AdamsCM,etal.TheDiscoveryofN-(1-Methyl-5-(trifluoromethyl)-1H-pyrazol-3-yl)-5-((6-((methylamino)methyl)pyrimidin-4-yl)oxy)-1H-indole-1-carboxamide(Acrizanib),aVEGFR-2InhibitorSpecificallyDesignedforTopicalOcularDelivery,asaTherapyforMcePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresear